Abiraterone Acetate (CAS 154229-18-2) is a synthetic androstane steroid derivative and the 3β-acetate ester of abiraterone, formally created by the condensation of the 3β-hydroxy group of abiraterone with acetic acid. This esterification enhances the drug's oral bioavailability compared to its active form, abiraterone.
Abiraterone Acetate is a pivotal pharmaceutical intermediate, API, and analytical reference standard in the treatment of prostate cancer, functioning as an orally active acetate ester prodrug of the steroidal compound abiraterone with potent antiandrogen activity. As a prodrug, Abiraterone Acetate is rapidly converted in vivo to abiraterone, which inhibits the enzymatic activity of steroid 17α-monooxygenase (17α-hydroxylase/C17,20-lyase complex; CYP17A1), a member of the cytochrome P450 family that catalyzes the 17α-hydroxylation of steroid intermediates involved in testosterone synthesis. Abiraterone Acetate suppresses testosterone production by both the testes and the adrenals to castrate-range levels, demonstrating significant antitumor activity in post-docetaxel patients with CRPC. Abiraterone Acetate is supplied with detailed characterization data and serves as both the API for commercial Zytiga® production and a reference standard for analytical method development and quality control applications. Abiraterone Acetate possesses a melting point of 144–145 °C and appears as a white to off-white, crystalline solid.
Product Parameters
Parameter
Specification
Product Name
Abiraterone Acetate
CAS Number
154229-18-2
Molecular Formula
C₂₆H₃₃NO₂
Molecular Weight
391.55 g/mol
Appearance
White to off-white, crystalline solid
Melting Point
127-130 °C
Boiling Point
506.7±50.0 °C
Storage Condition
–20 °C
Mechanism Of Action
Abiraterone acetate is an orally effective CYP17 inhibitor that is metabolized in vivo into abiraterone for therapeutic action, exhibiting 10–30 times greater inhibitory potency against 17α-hydroxylase/C17,20-lactonase (CYP17) than ketoconazole. Clinical studies have demonstrated that abiraterone acetate significantly reduces prostate-specific antigen (PSA) levels in prostate cancer patients, promotes tumor shrinkage, and extends survival by several years in advanced-stage patients. Abiraterone acetate serves as the prodrug of abiraterone and acts as a targeted agent targeting the androgen receptor signaling pathway. Abiraterone itself is a highly selective and potent inhibitor of cytochrome oxidase CYP17 with irreversible inhibitory effects, which are 10–30 times stronger than those of the non-selective inhibitor ketoconazole.
Application
Abiraterone acetate is a CYP17 inhibitor that, when combined with prednisone, can be used to treat prostate cancer patients who have previously received docetaxel chemotherapy for metastatic disease. As a precursor chemical compound, abiraterone acetate is converted in the body into abiraterone, an androgen biosynthesis inhibitor that exerts its therapeutic effect by inhibiting the activity of the CYP17 enzyme and thereby suppressing androgen biosynthesis.
Physicochemical Property
Abiraterone acetate is a CYP17 inhibitor indicated for use in combination with prednisone in the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel-based chemotherapy.
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